| Name | BAY-218 |
| Description | Bindarit (AF2838)is an aryl hydrocarbon receptor (AHR) antagonist with IC50 of 39.9 nM in the human glioblastoma U87 cell line. BAY-218 inhibition of AhR stimulates pro-inflammatory monocyte and T cell responses in vitro and drives anti-tumor immune responses, leading to reduced tumor growth in vivo. |
| In vitro | METHODS: Human monocytic U937 cells were treated with BAY-218 (AHR antagonist 1)(1 nM, 3nM, 10nM, 30nM, 100nM, 300nM, 1 μΜ and 3μΜ) and the IC50 values were determined.
RESULTS BAY-218 exhibited CYP1A1 inhibitory activity with an IC50 of 70.7 μM in the human monocytic U937 cell line. [1]
METHODS: BAY-218 (72 pM, 0.25 nM, 0.89 nM; 3.1 nM, 1 1 nM, 38 nM, 130 nM, 470 nM, 1.6 pM, 5.7 p, 20 μM) was used to treat U87 glioblastoma cells endogenously expressing AHR and the IC50 value was determined.
RESULTS BAY-218 could inhibit the activity of AHR in U87 glioblastoma cells with an IC50 of 39.9 μM. [1] |
| In vivo | METHODS: Bindarit (AF2838)(30 mg/kg, oral, twice daily) and aPD-L1 (10 mg/kg, intraperitoneal injection, twice daily) were used to treat mice with CT26 tumor cell xenografts injected subcutaneously in the flank to observe their anti-tumor ability.
RESULTS Combination therapy of BAY-218 and aPD-L1 inhibited tumor growth in mice. [1] |
| Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 250 mg/mL (622.17 mM)
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| Keywords | cancer | human monocytic U937 cells | AHR antagonist1 | inhibit | BAY-218 | Aryl Hydrocarbon Receptor | Inhibitor | BAY 218 | aryl hydrocarbon receptor (AHR) | U87 glioblastoma cells | AHR antagonist-1 | immune | BAY218 | AhR |
| Inhibitors Related | Nimodipine | Carbidopa monohydrate | Diosmin | (-)-Perillaldehyde | Prochloraz | Benzyl butyl phthalate | Skatole | L-Kynurenine | Indole-3-carbinol | MeBIO | Leflunomide | Mexiletine hydrochloride |
| Related Compound Libraries | Nonsteroidal Anti-Inflammatory Compound Library | Nuclear Receptor Compound Library | Bioactive Compound Library | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Transcription Factor-Targeted Compound Library |
United States
